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Progettazione, sintesi e attività anti-HIV degli analoghi della curcumina

Progettazione, sintesi e attività anti-HIV degli analoghi della curcumina

Mohamed Jawed Ahsan / Sachin Kumar Sharma

58,88 €
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Editorial:
KS OmniScriptum Publishing
Año de edición:
2025
Materia
Farmacología
ISBN:
9786209358456
58,88 €
IVA incluido
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Una serie di 11 analoghi della curcumina è stata sottoposta a previsione delle proprietà molecolari e somiglianza farmacologica mediante i software Molinspiration e MolSoft, nonché a parametri di lipofilia e solubilità utilizzando il programma ALOGPS 2.1. I composti che seguivano la 'Regola dei cinque' di Lipinski sono stati sintetizzati per lo screening anti-HIV come farmaci/principi attivi biodisponibili per via orale. Successivamente, la struttura dei composti sintetizzati è stata confermata da analisi spettrali (IR, NMR e massa) e i composti (3a-k) sono stati valutati per l’attività anti-HIV secondo il protocollo standard. Il punteggio massimo del modello di somiglianza farmacologica (1.1.0) è stato riscontrato per il 3,5-bis(4-idrossi-3-metilstiril)-N-(4-clorofenil)-1H-pirazolo-1-carbossamide (3b). Il composto 3b ha dimostrato attività anti-HIV con IC50 >3,71 µM e CC50 3,71 µM, tuttavia l’attività è risultata inferiore a quella del farmaco standard zidovudina.

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